Compounds > pf 956980
Page last updated: 2024-11-13

pf 956980

Description

PF 956980: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

PF-956980 : A pyrrolopyrimidine that is 7H-pyrrolo[2,3-d]pyrimidine substituted at position 4 by a methyl[(3R,4R)-4-methyl-1-(pyrrolidin-1-ylcarbonyl)piperidin-3-yl]nitrilo group. It is a potent JAK3-selective chemical probe. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID53344620
CHEMBL ID4068357
CHEBI ID144672
SCHEMBL ID15496537
MeSH IDM0553490

Synonyms (18)

Synonym
pf 956980
pfe-pkis 8
1262832-74-5
{(3r,4r)-4-methyl-3-[methyl(7h-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl}(pyrrolidin-1-yl)methanone
pf-956980
pf956980
CHEBI:144672
SCHEMBL15496537
((3r,4r)-4-methyl-3-(methyl(7h-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)(pyrrolidin-1-yl)methanone
7gv ,
[(3r,4r)-4-methyl-3-[methyl(7h-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]-pyrrolidin-1-ylmethanone
NCGC00386721-01
bdbm50234898
CHEMBL4068357 ,
pf-00956980
gtpl11060
NCGC00386721-02
E99050

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)		0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitorAn EC 2.7.10.* (protein-tyrosine kinase) inhibitor that specifically blocks the action of non-specific protein-tyrosine kinase (EC 2.7.10.2).
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (4)

ClassDescription
pyrrolopyrimidine
tertiary amino compoundA compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups.
N-acylpiperidine
N-acylpyrrolidine
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (8)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
PPM1D proteinHomo sapiens (human)Potency16.53880.00529.466132.9993AID1347411
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency5.35470.01237.983543.2770AID1645841
cytochrome P450 2D6Homo sapiens (human)Potency26.83700.00108.379861.1304AID1645840
Interferon betaHomo sapiens (human)Potency16.53880.00339.158239.8107AID1347411
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Tyrosine-protein kinase JAK2Homo sapiens (human)IC50 (µMol)0.05260.00010.372210.0000AID1436130; AID1436133; AID1673897
Tyrosine-protein kinase JAK1Homo sapiens (human)IC50 (µMol)0.02400.00030.23787.3000AID1436131; AID1436133; AID1673896
Non-receptor tyrosine-protein kinase TYK2Homo sapiens (human)IC50 (µMol)0.59570.00020.29504.1000AID1436127; AID1436133; AID1673899
Tyrosine-protein kinase JAK3Homo sapiens (human)IC50 (µMol)0.05640.00010.41937.9200AID1436129; AID1436133; AID1673898
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (146)

Processvia Protein(s)Taxonomy
positive regulation of platelet aggregationTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of platelet activationTyrosine-protein kinase JAK2Homo sapiens (human)
response to antibioticTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of SMAD protein signal transductionTyrosine-protein kinase JAK2Homo sapiens (human)
microglial cell activationTyrosine-protein kinase JAK2Homo sapiens (human)
adaptive immune responseTyrosine-protein kinase JAK2Homo sapiens (human)
chromatin remodelingTyrosine-protein kinase JAK2Homo sapiens (human)
transcription by RNA polymerase IITyrosine-protein kinase JAK2Homo sapiens (human)
protein phosphorylationTyrosine-protein kinase JAK2Homo sapiens (human)
apoptotic processTyrosine-protein kinase JAK2Homo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processTyrosine-protein kinase JAK2Homo sapiens (human)
immune responseTyrosine-protein kinase JAK2Homo sapiens (human)
signal transductionTyrosine-protein kinase JAK2Homo sapiens (human)
enzyme-linked receptor protein signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
G protein-coupled receptor signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationTyrosine-protein kinase JAK2Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STATTyrosine-protein kinase JAK2Homo sapiens (human)
tyrosine phosphorylation of STAT proteinTyrosine-protein kinase JAK2Homo sapiens (human)
mesoderm developmentTyrosine-protein kinase JAK2Homo sapiens (human)
negative regulation of cell population proliferationTyrosine-protein kinase JAK2Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to oxidative stressTyrosine-protein kinase JAK2Homo sapiens (human)
negative regulation of cardiac muscle cell apoptotic processTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of cell-substrate adhesionTyrosine-protein kinase JAK2Homo sapiens (human)
response to amineTyrosine-protein kinase JAK2Homo sapiens (human)
peptidyl-tyrosine phosphorylationTyrosine-protein kinase JAK2Homo sapiens (human)
cytokine-mediated signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
negative regulation of cell-cell adhesionTyrosine-protein kinase JAK2Homo sapiens (human)
actin filament polymerizationTyrosine-protein kinase JAK2Homo sapiens (human)
cell differentiationTyrosine-protein kinase JAK2Homo sapiens (human)
erythrocyte differentiationTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of cell migrationTyrosine-protein kinase JAK2Homo sapiens (human)
axon regenerationTyrosine-protein kinase JAK2Homo sapiens (human)
intracellular mineralocorticoid receptor signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of insulin secretionTyrosine-protein kinase JAK2Homo sapiens (human)
response to lipopolysaccharideTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of type II interferon productionTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of interleukin-1 beta productionTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of interleukin-17 productionTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of tumor necrosis factor productionTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of natural killer cell proliferationTyrosine-protein kinase JAK2Homo sapiens (human)
response to hydroperoxideTyrosine-protein kinase JAK2Homo sapiens (human)
tumor necrosis factor-mediated signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
symbiont-induced defense-related programmed cell deathTyrosine-protein kinase JAK2Homo sapiens (human)
response to tumor necrosis factorTyrosine-protein kinase JAK2Homo sapiens (human)
post-embryonic hemopoiesisTyrosine-protein kinase JAK2Homo sapiens (human)
intracellular signal transductionTyrosine-protein kinase JAK2Homo sapiens (human)
interleukin-12-mediated signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
cellular response to interleukin-3Tyrosine-protein kinase JAK2Homo sapiens (human)
interleukin-5-mediated signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
collagen-activated signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
interleukin-3-mediated signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
granulocyte-macrophage colony-stimulating factor signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of T cell proliferationTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of protein import into nucleusTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of tyrosine phosphorylation of STAT proteinTyrosine-protein kinase JAK2Homo sapiens (human)
activation of Janus kinase activityTyrosine-protein kinase JAK2Homo sapiens (human)
negative regulation of DNA bindingTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of MAPK cascadeTyrosine-protein kinase JAK2Homo sapiens (human)
negative regulation of neuron apoptotic processTyrosine-protein kinase JAK2Homo sapiens (human)
post-translational protein modificationTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of MHC class II biosynthetic processTyrosine-protein kinase JAK2Homo sapiens (human)
regulation of nitric oxide biosynthetic processTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of nitric oxide biosynthetic processTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of cell differentiationTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of transcription by RNA polymerase IITyrosine-protein kinase JAK2Homo sapiens (human)
regulation of receptor signaling pathway via JAK-STATTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of receptor signaling pathway via JAK-STATTyrosine-protein kinase JAK2Homo sapiens (human)
protein autophosphorylationTyrosine-protein kinase JAK2Homo sapiens (human)
platelet-derived growth factor receptor signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
regulation of inflammatory responseTyrosine-protein kinase JAK2Homo sapiens (human)
modulation of chemical synaptic transmissionTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of NK T cell proliferationTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of nitric-oxide synthase biosynthetic processTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionTyrosine-protein kinase JAK2Homo sapiens (human)
type II interferon-mediated signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
growth hormone receptor signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
growth hormone receptor signaling pathway via JAK-STATTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of growth hormone receptor signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
mammary gland epithelium developmentTyrosine-protein kinase JAK2Homo sapiens (human)
interleukin-6-mediated signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of leukocyte proliferationTyrosine-protein kinase JAK2Homo sapiens (human)
response to interleukin-12Tyrosine-protein kinase JAK2Homo sapiens (human)
interleukin-35-mediated signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
cellular response to lipopolysaccharideTyrosine-protein kinase JAK2Homo sapiens (human)
cellular response to dexamethasone stimulusTyrosine-protein kinase JAK2Homo sapiens (human)
extrinsic apoptotic signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
cellular response to virusTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of cold-induced thermogenesisTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of growth factor dependent skeletal muscle satellite cell proliferationTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of epithelial cell apoptotic processTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of vascular associated smooth muscle cell proliferationTyrosine-protein kinase JAK2Homo sapiens (human)
regulation of postsynapse to nucleus signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of signaling receptor activityTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of T-helper 17 type immune responseTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of apoptotic signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
regulation of apoptotic processTyrosine-protein kinase JAK2Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
response to antibioticTyrosine-protein kinase JAK1Homo sapiens (human)
protein phosphorylationTyrosine-protein kinase JAK1Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STATTyrosine-protein kinase JAK1Homo sapiens (human)
cytokine-mediated signaling pathwayTyrosine-protein kinase JAK1Homo sapiens (human)
positive regulation of homotypic cell-cell adhesionTyrosine-protein kinase JAK1Homo sapiens (human)
interleukin-15-mediated signaling pathwayTyrosine-protein kinase JAK1Homo sapiens (human)
interleukin-4-mediated signaling pathwayTyrosine-protein kinase JAK1Homo sapiens (human)
interleukin-2-mediated signaling pathwayTyrosine-protein kinase JAK1Homo sapiens (human)
interleukin-9-mediated signaling pathwayTyrosine-protein kinase JAK1Homo sapiens (human)
interleukin-11-mediated signaling pathwayTyrosine-protein kinase JAK1Homo sapiens (human)
type III interferon-mediated signaling pathwayTyrosine-protein kinase JAK1Homo sapiens (human)
type II interferon-mediated signaling pathwayTyrosine-protein kinase JAK1Homo sapiens (human)
type I interferon-mediated signaling pathwayTyrosine-protein kinase JAK1Homo sapiens (human)
interleukin-6-mediated signaling pathwayTyrosine-protein kinase JAK1Homo sapiens (human)
T-helper 17 cell lineage commitmentTyrosine-protein kinase JAK1Homo sapiens (human)
cellular response to virusTyrosine-protein kinase JAK1Homo sapiens (human)
interleukin-10-mediated signaling pathwayTyrosine-protein kinase JAK1Homo sapiens (human)
protein localization to cell-cell junctionTyrosine-protein kinase JAK1Homo sapiens (human)
positive regulation of protein localization to nucleusTyrosine-protein kinase JAK1Homo sapiens (human)
positive regulation of sprouting angiogenesisTyrosine-protein kinase JAK1Homo sapiens (human)
intracellular signal transductionTyrosine-protein kinase JAK1Homo sapiens (human)
tyrosine phosphorylation of STAT proteinTyrosine-protein kinase JAK1Homo sapiens (human)
cell differentiationTyrosine-protein kinase JAK1Homo sapiens (human)
growth hormone receptor signaling pathway via JAK-STATTyrosine-protein kinase JAK1Homo sapiens (human)
protein phosphorylationNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
immune responseNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STATNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
cytokine-mediated signaling pathwayNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
positive regulation of type II interferon productionNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
positive regulation of interleukin-17 productionNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
positive regulation of natural killer cell proliferationNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
interleukin-12-mediated signaling pathwayNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
type III interferon-mediated signaling pathwayNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
positive regulation of T cell proliferationNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
positive regulation of receptor signaling pathway via JAK-STATNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
positive regulation of NK T cell proliferationNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
type II interferon-mediated signaling pathwayNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
type I interferon-mediated signaling pathwayNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
cellular response to virusNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
interleukin-10-mediated signaling pathwayNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
positive regulation of protein localization to nucleusNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
positive regulation of T-helper 17 type immune responseNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
intracellular signal transductionNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
cell differentiationNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
growth hormone receptor signaling pathway via JAK-STATNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
adaptive immune responseTyrosine-protein kinase JAK3Homo sapiens (human)
negative regulation of dendritic cell cytokine productionTyrosine-protein kinase JAK3Homo sapiens (human)
protein phosphorylationTyrosine-protein kinase JAK3Homo sapiens (human)
enzyme-linked receptor protein signaling pathwayTyrosine-protein kinase JAK3Homo sapiens (human)
tyrosine phosphorylation of STAT proteinTyrosine-protein kinase JAK3Homo sapiens (human)
peptidyl-tyrosine phosphorylationTyrosine-protein kinase JAK3Homo sapiens (human)
B cell differentiationTyrosine-protein kinase JAK3Homo sapiens (human)
negative regulation of interleukin-10 productionTyrosine-protein kinase JAK3Homo sapiens (human)
negative regulation of interleukin-12 productionTyrosine-protein kinase JAK3Homo sapiens (human)
intracellular signal transductionTyrosine-protein kinase JAK3Homo sapiens (human)
interleukin-15-mediated signaling pathwayTyrosine-protein kinase JAK3Homo sapiens (human)
interleukin-4-mediated signaling pathwayTyrosine-protein kinase JAK3Homo sapiens (human)
interleukin-2-mediated signaling pathwayTyrosine-protein kinase JAK3Homo sapiens (human)
interleukin-9-mediated signaling pathwayTyrosine-protein kinase JAK3Homo sapiens (human)
T cell homeostasisTyrosine-protein kinase JAK3Homo sapiens (human)
innate immune responseTyrosine-protein kinase JAK3Homo sapiens (human)
negative regulation of FasL productionTyrosine-protein kinase JAK3Homo sapiens (human)
negative regulation of T-helper 1 cell differentiationTyrosine-protein kinase JAK3Homo sapiens (human)
regulation of receptor signaling pathway via JAK-STATTyrosine-protein kinase JAK3Homo sapiens (human)
negative regulation of T cell activationTyrosine-protein kinase JAK3Homo sapiens (human)
growth hormone receptor signaling pathway via JAK-STATTyrosine-protein kinase JAK3Homo sapiens (human)
regulation of T cell apoptotic processTyrosine-protein kinase JAK3Homo sapiens (human)
negative regulation of thymocyte apoptotic processTyrosine-protein kinase JAK3Homo sapiens (human)
response to interleukin-2Tyrosine-protein kinase JAK3Homo sapiens (human)
response to interleukin-4Tyrosine-protein kinase JAK3Homo sapiens (human)
response to interleukin-15Tyrosine-protein kinase JAK3Homo sapiens (human)
response to interleukin-9Tyrosine-protein kinase JAK3Homo sapiens (human)
regulation of apoptotic processTyrosine-protein kinase JAK3Homo sapiens (human)
cell differentiationTyrosine-protein kinase JAK3Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STATTyrosine-protein kinase JAK3Homo sapiens (human)
cytokine-mediated signaling pathwayTyrosine-protein kinase JAK3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (27)

Processvia Protein(s)Taxonomy
protein kinase activityTyrosine-protein kinase JAK2Homo sapiens (human)
protein tyrosine kinase activityTyrosine-protein kinase JAK2Homo sapiens (human)
non-membrane spanning protein tyrosine kinase activityTyrosine-protein kinase JAK2Homo sapiens (human)
signaling receptor bindingTyrosine-protein kinase JAK2Homo sapiens (human)
growth hormone receptor bindingTyrosine-protein kinase JAK2Homo sapiens (human)
interleukin-12 receptor bindingTyrosine-protein kinase JAK2Homo sapiens (human)
protein bindingTyrosine-protein kinase JAK2Homo sapiens (human)
ATP bindingTyrosine-protein kinase JAK2Homo sapiens (human)
protein kinase bindingTyrosine-protein kinase JAK2Homo sapiens (human)
heme bindingTyrosine-protein kinase JAK2Homo sapiens (human)
type 1 angiotensin receptor bindingTyrosine-protein kinase JAK2Homo sapiens (human)
acetylcholine receptor bindingTyrosine-protein kinase JAK2Homo sapiens (human)
histone H3Y41 kinase activityTyrosine-protein kinase JAK2Homo sapiens (human)
SH2 domain bindingTyrosine-protein kinase JAK2Homo sapiens (human)
histone bindingTyrosine-protein kinase JAK2Homo sapiens (human)
identical protein bindingTyrosine-protein kinase JAK2Homo sapiens (human)
phosphatidylinositol 3-kinase bindingTyrosine-protein kinase JAK2Homo sapiens (human)
insulin receptor substrate bindingTyrosine-protein kinase JAK2Homo sapiens (human)
metal ion bindingTyrosine-protein kinase JAK2Homo sapiens (human)
peptide hormone receptor bindingTyrosine-protein kinase JAK2Homo sapiens (human)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
protein tyrosine kinase activityTyrosine-protein kinase JAK1Homo sapiens (human)
non-membrane spanning protein tyrosine kinase activityTyrosine-protein kinase JAK1Homo sapiens (human)
growth hormone receptor bindingTyrosine-protein kinase JAK1Homo sapiens (human)
protein bindingTyrosine-protein kinase JAK1Homo sapiens (human)
ATP bindingTyrosine-protein kinase JAK1Homo sapiens (human)
protein phosphatase bindingTyrosine-protein kinase JAK1Homo sapiens (human)
ubiquitin protein ligase bindingTyrosine-protein kinase JAK1Homo sapiens (human)
CCR5 chemokine receptor bindingTyrosine-protein kinase JAK1Homo sapiens (human)
metal ion bindingTyrosine-protein kinase JAK1Homo sapiens (human)
protein tyrosine kinase activityNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
non-membrane spanning protein tyrosine kinase activityNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
growth hormone receptor bindingNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
protein bindingNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
ATP bindingNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
type 1 angiotensin receptor bindingNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
protein tyrosine kinase activityTyrosine-protein kinase JAK3Homo sapiens (human)
protein bindingTyrosine-protein kinase JAK3Homo sapiens (human)
ATP bindingTyrosine-protein kinase JAK3Homo sapiens (human)
protein phosphatase bindingTyrosine-protein kinase JAK3Homo sapiens (human)
growth hormone receptor bindingTyrosine-protein kinase JAK3Homo sapiens (human)
non-membrane spanning protein tyrosine kinase activityTyrosine-protein kinase JAK3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (23)

Processvia Protein(s)Taxonomy
extrinsic component of plasma membraneTyrosine-protein kinase JAK2Homo sapiens (human)
extrinsic component of cytoplasmic side of plasma membraneTyrosine-protein kinase JAK2Homo sapiens (human)
nucleusTyrosine-protein kinase JAK2Homo sapiens (human)
nucleoplasmTyrosine-protein kinase JAK2Homo sapiens (human)
cytoplasmTyrosine-protein kinase JAK2Homo sapiens (human)
cytosolTyrosine-protein kinase JAK2Homo sapiens (human)
cytoskeletonTyrosine-protein kinase JAK2Homo sapiens (human)
plasma membraneTyrosine-protein kinase JAK2Homo sapiens (human)
caveolaTyrosine-protein kinase JAK2Homo sapiens (human)
focal adhesionTyrosine-protein kinase JAK2Homo sapiens (human)
granulocyte macrophage colony-stimulating factor receptor complexTyrosine-protein kinase JAK2Homo sapiens (human)
endosome lumenTyrosine-protein kinase JAK2Homo sapiens (human)
interleukin-12 receptor complexTyrosine-protein kinase JAK2Homo sapiens (human)
membrane raftTyrosine-protein kinase JAK2Homo sapiens (human)
interleukin-23 receptor complexTyrosine-protein kinase JAK2Homo sapiens (human)
postsynapseTyrosine-protein kinase JAK2Homo sapiens (human)
glutamatergic synapseTyrosine-protein kinase JAK2Homo sapiens (human)
euchromatinTyrosine-protein kinase JAK2Homo sapiens (human)
cytosolTyrosine-protein kinase JAK2Homo sapiens (human)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
cytoplasmTyrosine-protein kinase JAK1Homo sapiens (human)
plasma membraneTyrosine-protein kinase JAK1Homo sapiens (human)
cytoplasmic side of plasma membraneTyrosine-protein kinase JAK1Homo sapiens (human)
extrinsic component of cytoplasmic side of plasma membraneTyrosine-protein kinase JAK1Homo sapiens (human)
nucleusTyrosine-protein kinase JAK1Homo sapiens (human)
cytoplasmTyrosine-protein kinase JAK1Homo sapiens (human)
endosomeTyrosine-protein kinase JAK1Homo sapiens (human)
cytosolTyrosine-protein kinase JAK1Homo sapiens (human)
cytoskeletonTyrosine-protein kinase JAK1Homo sapiens (human)
focal adhesionTyrosine-protein kinase JAK1Homo sapiens (human)
cytosolTyrosine-protein kinase JAK1Homo sapiens (human)
plasma membraneNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
cytoplasmic side of plasma membraneNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
extrinsic component of plasma membraneNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
extrinsic component of cytoplasmic side of plasma membraneNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
nucleusNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
cytoplasmNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
cytosolNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
cytoskeletonNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
plasma membraneNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
interleukin-12 receptor complexNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
extracellular exosomeNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
interleukin-23 receptor complexNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
cytosolNon-receptor tyrosine-protein kinase TYK2Homo sapiens (human)
extrinsic component of plasma membraneTyrosine-protein kinase JAK3Homo sapiens (human)
extrinsic component of cytoplasmic side of plasma membraneTyrosine-protein kinase JAK3Homo sapiens (human)
endosomeTyrosine-protein kinase JAK3Homo sapiens (human)
cytosolTyrosine-protein kinase JAK3Homo sapiens (human)
cytoskeletonTyrosine-protein kinase JAK3Homo sapiens (human)
plasma membraneTyrosine-protein kinase JAK3Homo sapiens (human)
cytosolTyrosine-protein kinase JAK3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (20)

Assay IDTitleYearJournalArticle
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1436131Inhibition of GST tagged human recombinant JAK1 catalytic domain expressed in baculovirus using peptide substrate preincubated for 60 mins followed by substrate addition and measured after 60 mins by microfluidic assay2017Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2
Design and Synthesis of a Pan-Janus Kinase Inhibitor Clinical Candidate (PF-06263276) Suitable for Inhaled and Topical Delivery for the Treatment of Inflammatory Diseases of the Lungs and Skin.
AID1673899Inhibition of human TYK2 using 5FAM-KKSRGDYMTMQID as substrate by caliper microfluidic mobility shift assay2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Monomeric Targeted Protein Degraders.
AID1436129Inhibition of GST tagged human recombinant JAK3 catalytic domain expressed in baculovirus using peptide substrate preincubated for 60 mins followed by substrate addition and measured after 60 mins by microfluidic assay2017Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2
Design and Synthesis of a Pan-Janus Kinase Inhibitor Clinical Candidate (PF-06263276) Suitable for Inhaled and Topical Delivery for the Treatment of Inflammatory Diseases of the Lungs and Skin.
AID1436128Metabolic stability in human liver microsomes assessed per mg protein2017Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2
Design and Synthesis of a Pan-Janus Kinase Inhibitor Clinical Candidate (PF-06263276) Suitable for Inhaled and Topical Delivery for the Treatment of Inflammatory Diseases of the Lungs and Skin.
AID1436130Inhibition of GST tagged human recombinant JAK2 catalytic domain expressed in baculovirus using peptide substrate preincubated for 60 mins followed by substrate addition and measured after 60 mins by microfluidic assay2017Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2
Design and Synthesis of a Pan-Janus Kinase Inhibitor Clinical Candidate (PF-06263276) Suitable for Inhaled and Topical Delivery for the Treatment of Inflammatory Diseases of the Lungs and Skin.
AID1436133Inhibition of JAK in human PBMC assessed as reduction in human recombinant IL-2/ mouse anti-human CD3 stimulated STAT5 phosphorylation at tyrosine residue preincubated for 1 hr followed by IL2/CD3 stimulation after 30 mins by immunofluorescence assay2017Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2
Design and Synthesis of a Pan-Janus Kinase Inhibitor Clinical Candidate (PF-06263276) Suitable for Inhaled and Topical Delivery for the Treatment of Inflammatory Diseases of the Lungs and Skin.
AID1436181Inhibition of JAK in human PBMC assessed as reduction in human recombinant IL-2/ mouse anti-human CD3 stimulated STAT5 phosphorylation at tyrosine residue at 10-fold IC50 preincubated for 1 hr followed by compound washout and subsequent IL2/CD3 stimulatio2017Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2
Design and Synthesis of a Pan-Janus Kinase Inhibitor Clinical Candidate (PF-06263276) Suitable for Inhaled and Topical Delivery for the Treatment of Inflammatory Diseases of the Lungs and Skin.
AID1673896Inhibition of human JAK1 using 5FAM-KKSRGDYMTMQID as substrate by caliper microfluidic mobility shift assay2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Monomeric Targeted Protein Degraders.
AID1673901Downregulation of JAK3 mRNA expression in human PBMC at 1 uM after 22 hrs by qPCR analysis relative to control2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Monomeric Targeted Protein Degraders.
AID1673897Inhibition of human JAK2 using FITC-KGGEEEEYFELVKK as substrate by caliper microfluidic mobility shift assay2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Monomeric Targeted Protein Degraders.
AID1673900Downregulation of JAK2 mRNA expression in human PBMC at 1 uM after 22 hrs by qPCR analysis relative to control2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Monomeric Targeted Protein Degraders.
AID1436140Drug metabolism in human liver microsomes assessed as UGT-mediated compound glucuronidation per mg protein in presence of microsomal activator Brij58 and cofactor UDPGA2017Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2
Design and Synthesis of a Pan-Janus Kinase Inhibitor Clinical Candidate (PF-06263276) Suitable for Inhaled and Topical Delivery for the Treatment of Inflammatory Diseases of the Lungs and Skin.
AID1673898Inhibition of human JAK3 using FITC-KGGEEEEYFELVKK as substrate by caliper microfluidic mobility shift assay2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Monomeric Targeted Protein Degraders.
AID1436127Inhibition of Tyk2 (unknown origin) using peptide substrate preincubated for 60 mins followed by substrate addition and measured after 60 mins by microfluidic assay2017Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2
Design and Synthesis of a Pan-Janus Kinase Inhibitor Clinical Candidate (PF-06263276) Suitable for Inhaled and Topical Delivery for the Treatment of Inflammatory Diseases of the Lungs and Skin.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (11)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (9.09)29.6817
2010's6 (54.55)24.3611
2020's4 (36.36)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 17.84

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index17.84 (24.57)
Research Supply Index2.48 (2.92)
Research Growth Index5.14 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (17.84)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (9.09%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other10 (90.91%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
4-(4'-hydroxyphenyl)-amino-6,7-dimethoxyquinazoline
WHI P131: a quinazoline derivative, inhibitor of glioblastoma cell adhesion and migration		2.0410
whi p154
WHI P154: an anti-leukemic agent; structure in first source		2.0410
pd 98059
2-(2-amino-3-methoxyphenyl)-4H-1-benzopyran-4-one: inhibits MAP kinase kinase (MEK) activity, p42 MAPK and p44 MAPK; structure in first source. 2-(2-amino-3-methoxyphenyl)chromen-4-one : A member of the class of monomethoxyflavones that is 3'-methoxyflavone bearing an additional amino substituent at position 2'.		2.0510aromatic amine;
monomethoxyflavone		EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
geroprotector
pyrroles
1H-pyrrole : A tautomer of pyrrole that has the double bonds at positions 2 and 4.. pyrrole : A five-membered monocyclic heteroarene comprising one NH and four CH units which forms the parent compound of the pyrrole group of compounds. Its five-membered ring structure has three tautomers. A 'closed class'.. azole : Any monocyclic heteroarene consisting of a five-membered ring containing nitrogen. Azoles can also contain one or more other non-carbon atoms, such as nitrogen, sulfur or oxygen.		4.0950pyrrole;
secondary amine
quinazolines
Quinazolines: A group of aromatic heterocyclic compounds that contain a bicyclic structure with two fused six-membered aromatic rings, a benzene ring and a pyrimidine ring.. quinazoline : A mancude organic heterobicyclic parent that is naphthalene in which the carbon atoms at positions 1 and 3 have been replaced by nitrogen atoms.. quinazolines : Any organic heterobicyclic compound based on a quinazoline skeleton and its substituted derivatives.		2.0410azaarene;
mancude organic heterobicyclic parent;
ortho-fused heteroarene;
quinazolines
artenimol
[no description available]		3.3510
tofacitinib
tofacitinib : A pyrrolopyrimidine that is pyrrolo[2,3-d]pyrimidine substituted at position 4 by an N-methyl,N-(1-cyanoacetyl-4-methylpiperidin-3-yl)amino moiety. Used as its citrate salt to treat moderately to severely active rheumatoid arthritis.		3.4320N-acylpiperidine;
nitrile;
pyrrolopyrimidine;
tertiary amino compound		antirheumatic drug;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor
cytochrome c-t
Cytochromes c: Cytochromes of the c type that are found in eukaryotic MITOCHONDRIA. They serve as redox intermediates that accept electrons from MITOCHONDRIAL ELECTRON TRANSPORT COMPLEX III and transfer them to MITOCHONDRIAL ELECTRON TRANSPORT COMPLEX IV.		2.0510
mln 8237
MLN 8237: an aurora kinase A inhibitor		3.3510benzazepine
piperidines
Piperidines: A family of hexahydropyridines.		310
lrrk2-in1
LRRK2-IN1: inhibits leucine-rich repeat kinase 2; structure in first source		3.3510aromatic amine;
aromatic ether;
N-acylpiperidine;
N-alkylpiperazine;
pyrimidobenzodiazepine;
secondary amino compound;
tertiary amino compound		antineoplastic agent;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor
azd3514
AZD3514: in Phase I clinical trial in patients with castrate-resistant prostate cancer (2/2013); structure in first source		3.3510
gne-7915
[no description available]		3.3510
gne-0877
2-methyl-2-(3-methyl-4-((4-(methylamino)-5-(trifluoromethyl)pyrimidin-2-yl)amino)-1H-pyrazol-1-yl)propanenitrile: a leucine-rich repeat kinase 2 (LRRK2) inhibitor; structure in first source		3.3510
9-(1-methyl-4-pyrazolyl)-1-[1-(1-oxoprop-2-enyl)-2,3-dihydroindol-6-yl]-2-benzo[h][1,6]naphthyridinone
[no description available]		3.3510naphthyridine derivative
MLI-2
MLI-2 : A member of the class of indazoles that is 1H-indazole that is substituted at position 3 by a 6-(cis-2,6-dimethylmorpholin-4-yl)pyrimidin-4-yl group and at position 5 by a (1-methylcyclopropoxy)group. It is an inhibitor of leucine-rich repeat kinase 2 (LRRK2).		3.3510aromatic ether;
cyclopropanes;
indazoles;
morpholines;
pyrimidines;
tertiary amino compound		EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor
ConditionIndicatedRelationship StrengthStudiesTrials
Disease, Pulmonary
[description not available]		02.1510
Dermatoses
[description not available]		02.1510
Lung Diseases
Pathological processes involving any part of the LUNG.		02.1510
Skin Diseases
Diseases involving the DERMIS or EPIDERMIS.		02.1510
Congenital Zika Syndrome
[description not available]		02.2510
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.2510
Zika Virus Infection
A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.		02.2510
Rheumatoid Arthritis
[description not available]		03.3820
Arthritis, Rheumatoid
A chronic systemic disease, primarily of the joints, marked by inflammatory changes in the synovial membranes and articular structures, widespread fibrinoid degeneration of the collagen fibers in mesenchymal tissues, and by atrophy and rarefaction of bony structures. Etiology is unknown, but autoimmune mechanisms have been implicated.		03.3820
B-Cell Chronic Lymphocytic Leukemia
[description not available]		02.0510
Leukemia, Lymphocytic, Chronic, B-Cell
A chronic leukemia characterized by abnormal B-lymphocytes and often generalized lymphadenopathy. In patients presenting predominately with blood and bone marrow involvement it is called chronic lymphocytic leukemia (CLL); in those predominately with enlarged lymph nodes it is called small lymphocytic lymphoma. These terms represent spectrums of the same disease.		02.0510
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